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CPG a metalloenzyme derived from
2020-11-28
CPG2, a metalloenzyme derived from sp., was the elected enzyme for the first pilot-scale clinical trial of ADEPT. This enzyme has no mammalian homologue and activates glutamic AG-221 prodrug derivatives of several nitrogen mustards alkylating agents., , , , , A bond cleavable by CPG2 is essential
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br Materials and methods br
2020-11-28
Materials and methods Results Discussion Recently it has been found that prostaglandins play an important role in modulating the host immune system [1,3,22,23], and some parasites produce these eicosanoid mediators to survive into their hosts [6,[10], [11], [12],24,25]. The discovery that p
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We then analyzed Ki proliferation index as a categorical var
2020-11-27
We then analyzed Ki-67 proliferation index as a categorical variable by using 15%, essentially the median Ki-67 value in the entire study group (see above), to delineate low and high proliferation subgroups. By Fisher's exact test, both the type 1 versus non-type 1 EWS-FLI1 comparison (P = 0.047; Ta
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br Introduction Hematopoietic stem cells and leukemic stem c
2020-11-27
Introduction Hematopoietic stem DHEA and leukemic stem cells (HSCs and LSCs, respectively) both have a capacity of self-renewal. Whereas HSCs give rise to all blood lineages during lifetime hematopoiesis, LSCs are responsible for the initiation and propagation of leukemia, as well as drug resista
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If the effects described here are present
2020-11-27
If the effects described here are present in catalysis, their empirical confirmation poses many challenges. Cat state correlations are fragile outside an environment especially suited for their preservation. As present day observational techniques whether in vivo or in vitro were not designed bearin
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In regards to regional variation in metabolic behavior of
2020-11-27
In regards to regional variation in metabolic behavior of adipose tissue, subcutaneous adipose tissue transplantation has been shown to reprogram visceral adipose tissue to have subcutaneous-like phenotypic behavior, whereas visceral-to-subcutaneous transplantation does not promote a more detrimenta
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The discoidin domain receptors DDR and DDR
2020-11-27
The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati
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During the host response to inflammation inflammatory mediat
2020-11-27
During the host response to inflammation, inflammatory mediators, including release of pro-inflammatory cytokines, have been associated with altered content, expression, and activity of CYP450 enzymes, consequently leading to alterations in the metabolism and elimination of certain drugs. The losses
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In conclusion we have shown that the cellular effects
2020-11-27
In conclusion, we have shown that the cellular effects produced by SFN in NSCLC CL 316243 disodium salt are largely mediated by SFN-induced production of ROS. Cells with higher levels of EGFR were more resistant to SFN treatment and showed resistance to SFN-induced apoptosis, suggesting that high E
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Other GPCRs notable for changes in expression on CLL cells
2020-11-27
Other GPCRs notable for changes in expression on CLL cells include upregulation of the thromboxane A2 receptor TBXA2R mRNA [61] and up and downregulation of mRNA and protein from the neurotensin receptors NTSR2 and NTSR1, respectively [62]. The Eμ-TCL1 mouse model of CLL has been used to study mult
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br Methods br Results br
2020-11-27
Methods Results Discussion Preclinical data indicate that nepicastat modulates sympathetic drive to the atp gamma s with a mild pressor effect in various animal models of hypertension (Stanney et al., 1998). However in this clinical study, the doses of nepicastat employed did not significa
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In light of the overall loss
2020-11-27
In light of the overall loss of activity and selectivity observed with this series of arylchromenone-4-ones bearing small -alkoxy substituents, we were pleased to identify a potent and relatively selective inhibitor , exhibiting IC values of 0.008μM and 0.07μM for DNA-PK and PI3Kα, respectively. The
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naphthalimide a well known DNA intercalator has been
2020-11-27
1,8-naphthalimide, a well-known DNA intercalator, has been extensively investigated in the development of antitumor agents [10]. Some of the naphthalimide derivatives, such as amonafide, elinafide and bisnafide (Fig. 1), have entered into phase II clinical trials stage [10]b), [11]. Among them, elin
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High throughput screening HTS of
2020-11-26
High throughput screening (HTS) of the AstraZeneca Milrinone collection was conducted and identified oxadiazole amide () originating from a kinase directed screening library (although inactive against a panel of kinases). This compound had moderate potency as a DGAT-1 inhibitor (IC=0.52μM) and was
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Recently Schenck et al identified an active site asparagine
2020-11-26
Recently, Schenck et al. [25] identified an active site asparagine 222 (N222) residue in the Glycine max TyrAp/PDH (GmPDH1) that is responsible for its prephenate substrate specificity. Mutating the single N222 into an acidic residue (i.e. aspartate, D) in the legume TyrAp/PDH shifted from prephenat
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